EPIGENE THERAPEUTICS INC. announces presentations on NEO2734, an oral dual inhibitor of both BET and CBP-P300, at the ASH 2018 Congress
- Category: Small Molecules
- Published on Tuesday, 04 December 2018 18:22
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Data demonstrate activity of NEO2734, with superior effects to those of standard BET inhibitors, in diffuse large B cell lymphomas.
MONTREAL, Canada I December 3, 2018 I Epigene Therapeutics Inc. announces that data on NEO2734, its investigational, first-in-class, dual inhibitor of both the Bromodomain and Extra-Terminal domain (BET) family of proteins and the Cyclic AMP response element binding protein (CREB)-binding protein (CBP) and E1A interacting protein of 300 kDa (EP300 or P300) will be presented at the American Society of Hematology (ASH) 2018 Congress taking place in San Diego, USA from November 30th to December 4th , 2018. The data being presented at ASH 2018 will include a poster presentation on NEO2734 activity in a broad array of pre-clinical models of diffuse large B cell lymphomas (DLBCL).
"Epigenetic changes within the lymphoproliferative disorders (LPD) are well established to be key drivers of these malignancies and a subset of defined developmental therapeutics targets have emerged", stated Dr. Francesco Bertoni, Università della Svizzera Italiana, Institute of Oncology Research, Bellinzona, Switzerland. "Our group has devoted significant pre-clinical and clinical efforts to maximizing the potential value of the traditional BET inhibitors in the full spectrum of lymphomas, with a particular focus on DLBCL, where we still have a major need for novel therapies. The activity of BET inhibitors is clear – as is the fact that this class of agents will need the addition of other agents or approaches with different modes of action and different susceptibilities to resistance to be of significant value in the LPD. Our data, being presented at this ASH meeting, showing the consistent superiority of NEO2734 over an array of both BET inhibitors and CBP-P300 inhibitors is exciting. These data were generated in a comprehensive panel of cell lines representing the broad molecular heterogeneity of DLBCL and are of immediate potential clinical relevance."
"We have invested heavily in the clinical exploration of the BET inhibitors in patients with DLBCL and consistently been both encouraged at clear activity and frustrated at the inability to achieve sufficient impact to define approvable single agent regimens" said Dr. Anastasios Stathis, Oncology Institute of Southern Switzerland, Bellinzona, Switzerland; "NEO2734 is a unique agent having the ability, with a single approach, to modulate multiple established targets in the LPD. I am also very excited about the positive data being generated on NEO2734 in NUT Carcinoma – an extremely aggressive cancer in which we also have clear evidence of pre-clinical activity of the traditional BET inhibitors. Our clinical experience with BET inhibitors in NUT Carcinoma has made it very clear that we need to modulate additional targets to make a meaningful clinical advance. I am thus particularly looking forward to enrolling patients with LPD or NUT Carcinoma on the initial NEO2734 clinical studies"
"The important data on DLBCL from our Bellinzona colleagues is another demonstration of the potential of delivering synergistic modulation of independent epigenetic targets in cancer" said Dr. Natalie Cook, Senior Clinical Lecturer in Experimental Cancer Medicine and Consultant in Medical Oncology at The Christie NHS Trust, University of Manchester, UK and member of the Epigene Therapeutics Scientific Advisory Board. "NEO2734 is unique in its ability to inhibit both the BET family and the CBP-P300 paralogs. The data in DLBCL is consistent with our observations on the relative activity of NEO2734 and traditional BET inhibitors in solid tumors including colon, prostate and lung cancers. With those traditional BET inhibitors, our clinical studies are increasingly focused on defining optimal complimentary approaches by adding other agents - NEO2734 may offer this necessary synergy within a single agent. We are very encouraged by the progress of NEO2734 towards the clinic and look forward to investigating its potential on international studies."
Targeting both BET and CREBBP/EP300 proteins with the novel dual inhibitor NEO2734 leads to more preclinical anti-tumor activity in diffuse large B cell lymphoma than with single BET or CREBBP/EP300 inhibitors. (Abstract #4174, poster display session 625. Lymphoma: Pre-Clinical—Chemotherapy and Biologic Agents: Hall GH (San Diego Convention Center)
-- Monday, 3 December 2018 from 18:00 p.m. PST to 20:00 p.m. PST
Full session details and data presentation listings for ASH 2018 can be found at:
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SOURCE: Epigene Therapeutics